“…In view of the potential therapeutic interest in CXCR3 blockade in diseases like rheumatoid arthritis and allograft rejection (Wijtmans et al, 2011), many different drug discovery programs have yielded several distinct chemical classes of small-molecule compounds, including antagonists as well as a few agonists (Wijtmans et al, 2008(Wijtmans et al, , 2011, such as the 8-azaquinazolinone compounds from Amgen Inc. (AMG487, (R)-N- (1-(3-(4-ethoxyphenyl)-4-oxo-3,4-dihydropyrido[2,3-d]pyrimidin-2-yl)ethyl)-N-(pyridin-3-ylmethyl)-2-(4-trifluoromethoxy)phenyl)acetamide; Washington, D.C.) and Neurocrine Biosciences pyrimidin-2-yl)ethyl)-2-(4-fluoro-3-(trifluoromethyl)phenyl)-N-(pyridin-3-ylmethyl)acetamide; San Diego, CA), which bind to CXCR3 with affinities in the nanomolar range (Heise et al, 2005;Johnson et al, 2007;Verzijl et al, 2008). Moreover, a piperazinyl-piperidine compound class containing ligands with nanomolar CXCR3 affinities was reported by Schering Plough (now Merck Sharp & Dohme, Kenilworth, NJ) (Mcguinness et al, 2009;Kim et al, 2011;Shao et al, 2011;Nair et al, 2014).…”